An inhibitor of Src and p38 MAPK kinases
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UM-164

Item No. 26188

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide
CAS Number
903564-48-7
Molecular Formula
C30H31F3N8O3S
Formula Weight
640.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 5 mg/ml
λmax
230, 324 nm
SMILES
O=C(NC1=CC=C(C)C(NC(C2=CN=C(NC3=NC(C)=NC(N4CCN(CCO)CC4)=C3)S2)=O)=C1)C5=CC(C(F)(F)F)=CC=C5
InChi Code
InChI=1S/C30H31F3N8O3S/c1-18-6-7-22(37-27(43)20-4-3-5-21(14-20)30(31,32)33)15-23(18)38-28(44)24-17-34-29(45-24)39-25-16-26(36-19(2)35-25)41-10-8-40(9-11-41)12-13-42/h3-7,14-17,42H,8-13H2,1-2H3,(H,37,43)(H,38,44)(H,34,35,36,39)
InChi Key
ANEBQUSWQAQFQB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).1 It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gilani, R.A., Phadke, S., Bao, L.W., et al. UM-164: A potent c-Src/p38 kinase inhibitor with in vivo activity against triple-negative breast cancer. Clin. Cancer Res. 22(20), 5087-5096 (2016).